公开(公告)号：WO2010010454A2

公开(公告)日：2010-01-28

申请号：PCT/IB2009/006347

申请日：2009-07-24

Applicant: MEDICHEM, S.A. ,  WINTER, Stephen, Benedict, David ,  BENITO VELEZ, Monica

Inventor： WINTER, Stephen, Benedict, David ,  BENITO VELEZ, Monica

IPC: C07D403/06 ,  A61K31/404 ,  A61P35/00

CPC classification number: C07D403/06

Abstract: Disclosed are crystalline polymorphic forms of the malic acid salt of (Z)-N-[2- (diethylamino)ethyl]-5-[(5-fluoro-l,2-dihydro-2-oxo-3H-indol-3-yliden)methyl]-2,4- dimethyl-1H-pyrrole-3-carboxamide, sunitinib malate, including crystalline Forms III, IV, V, VI and VII. Also disclosed are processes for preparing crystalline polymorphic forms of sunitinib malate and pharmaceutical compositions comprising sunitinib malate.

Abstract translation: 公开了（Z）-N- [2-（二乙基氨基）乙基] -5 - [（5-氟-1,2-二氢-2-甲基丙基）氨基]乙酸的苹果酸盐的结晶多晶型物， -3-羟基吲哚-3-亚基）甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺，苹果酸舒尼替尼，包括结晶形式III，IV，V，VI和VII。 还公开了用于制备苹果酸舒尼替尼的结晶多晶型物和包含苹果酸舒尼替尼的药物组合物的方法。

公开(公告)号：WO2009153649A1

公开(公告)日：2009-12-23

申请号：PCT/IB2009/005990

申请日：2009-06-19

Applicant: MEDICHEM, S.A. ,  SOLDEVILLA MADRID, Nuria

Inventor： SOLDEVILLA MADRID, Nuria

IPC: C07D207/16 ,  A61K31/40 ,  A61P13/10

CPC classification number: C07D207/06

Abstract: Disclosed is a process for preparing 3 -substituted pyrrolidine compounds of formula (VII) or salts thereof, wherein R1 is described herein, which are intermediate compounds useful for the synthesis of darifenacin which is indicated for the treatment of overactive bladder with symptoms of urge, urinary incontinence, and the like, and pharmaceutically acceptable salts thereof. Also disclosed is a process for preparing darifenacin and pharmaceutically acceptable salts thereof.

Abstract translation: 公开了一种制备式（VII）的3-取代吡咯烷化合物或其盐的方法，其中R 1在本文中描述，其是可用于合成达赖芬星的中间体化合物，其被指示用于治疗膀胱过度症状， 尿失禁等，及其药学上可接受的盐。 还公开了制备达赖芬那定及其药学上可接受的盐的方法。

公开(公告)号：WO2009109651A1

公开(公告)日：2009-09-11

申请号：PCT/EP2009/052654

申请日：2009-03-06

Applicant: MEDICHEM, S.A. ,  WINTER, Stephen, Benedict, David ,  BENITO VELEZ, Monica

Inventor： WINTER, Stephen, Benedict, David ,  BENITO VELEZ, Monica

IPC: C07D471/08

CPC classification number: C07D471/08

Abstract: This invention provides novel dicarboxylic acid salt forms of varenicline, wherein the acid is selected from maleic acid, fumaric acid, adipic acid, galactaric acid and malic acid. This invention provides also a carboxylic acid salt form of varenicline, wherein the acid is S-2-pyrrolidinon-5-carboxylic acid. This invention also provides methods for making these salt forms.

Abstract translation: 本发明提供了新的二甲酸盐形式的伐伦尼克林，其中酸选自马来酸，富马酸，己二酸，乳糖酸和苹果酸。 本发明还提供了伐伦碱的羧酸盐形式，其中酸是S-2-吡咯烷酮-5-羧酸。 本发明还提供了制备这些盐形式的方法。

公开(公告)号：WO2009074862A1

公开(公告)日：2009-06-18

申请号：PCT/IB2008/003458

申请日：2008-12-12

Applicant: MEDICHEM S.A. ,  WINTER, Stephen, Benedict, David ,  MANGION, Bernardino

Inventor： WINTER, Stephen, Benedict, David ,  MANGION, Bernardino

IPC: C07D403/06 ,  A61K31/405 ,  A61P35/00

CPC classification number: C07D403/06

Abstract: The invention relates to new crystalline polymorphic forms of N-[2- (diethylamino)ethyl]-5-[(Z)-(5-fluoro-l,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4- dimethyl-lH-pyrrole-3-carboxamide (i.e., sunitinib base), including Form I, Form II, and Form IV, processes for preparing crystalline polymorphic forms of sunitinib base, and pharmaceutically acceptable salts of new crystalline polymorphic forms of sunitinib base and pharmaceutical compositions comprising new crystalline polymorphic forms of sunitinib base, salts of new crystalline polymorphic forms of sunitinib base and mixtures thereof.

Abstract translation: 本发明涉及N- [2-（二乙基氨基）乙基] -5 - [（Z） - （5-氟-1,2-二氢-2-氧代-3H-吲哚-3-基） 甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺（即舒尼替尼碱），包括I型，II型和IV型，制备舒尼替尼碱的结晶多晶形式的方法和新的可药用盐 舒尼替尼碱的结晶多晶形式和包含舒尼替尼碱的新结晶多晶型形式的舒尼替尼碱的新结晶多晶形式的盐及其混合物的药物组合物。

公开(公告)号：WO2009031026A2

公开(公告)日：2009-03-12

申请号：PCT/IB2008/002319

申请日：2008-09-05

Applicant: MEDICHEM, S.A. ,  LLORET PEREZ, Sergio ,  PUIGVERT COLOMER, Marina

Inventor： LLORET PEREZ, Sergio ,  PUIGVERT COLOMER, Marina

IPC: A61K47/48

CPC classification number: B82Y5/00 ,  A61K47/6951

Abstract: The present invention relates to novel lamivudine/cyclodextrin complexes and processes for preparing said complexes. The present invention also relates to novel solid pharmaceutical compositions comprising lamivudine, wherein lamivudine is present in the form of said lamivudine/cyclodextrin complexes. The present invention further relates to processes for preparing said compositions.

Abstract translation: 本发明涉及新的拉米夫定/环糊精复合物及其制备方法。 本发明还涉及包含拉米夫定的新型固体药物组合物，其中拉米夫定以所述拉米夫定/环糊精复合物的形式存在。 本发明进一步涉及制备所述组合物的方法。

公开(公告)号：WO2008035212A2

公开(公告)日：2008-03-27

申请号：PCT/IB2007/003346

申请日：2007-06-08

Applicant: MEDICHEM, S.A. ,  SZEKERES, Tibor ,  RÉPÁSI, József ,  SZABÓ, András ,  MANGION, Bernardino

Inventor： SZEKERES, Tibor ,  RÉPÁSI, József ,  SZABÓ, András ,  MANGION, Bernardino

CPC classification number: C07C29/32 ,  C07C29/17 ,  C07C45/30 ,  C07C47/24 ,  C07C33/46 ,  C07C33/483

Abstract: The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates.

Abstract translation: 本发明一般涉及制备化合物（例如，3-（3-三氟甲基苯基）丙醛（下文化合物III））的改进方法，其是合成西那卡塞，其盐和/或溶剂合物的关键中间体 ，以及通过这种方法制备的这种化合物用于制备西那卡塞和/或其盐或溶剂合物的用途。

公开(公告)号：WO2007036771A2

公开(公告)日：2007-04-05

申请号：PCT/IB2006/001968

申请日：2006-05-05

Applicant: MEDICHEM, S.A. ,  AUQUER PEDEMONTE, Ignasi

Inventor： AUQUER PEDEMONTE, Ignasi

CPC classification number: C07D401/12

Abstract: The invention relates, in general, to a new solid crystalline form of pantoprazole free acid (denominated "Form III"), salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and methods for producing the same. The invention further includes formulating pantoprazole free acid Form III, salts derived therefrom (e.g., pantoprazole sodium and pantoprazole sodium sesquihydrate) and/or in vivo cleavable prodrugs thereof (collectively "the compounds of the invention") into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.

Abstract translation: 本发明一般涉及泮托拉唑游离酸的新固体形式（称为“形式III”），由其衍生的盐（例如泮托拉唑钠和泮托拉唑钠倍半水合物）及其制备方法。 本发明还包括将泮托拉唑游离酸形式III，衍生自其的盐（例如泮托拉唑钠和泮托拉唑钠倍半水合物）和/或其体内可切割的前药（统称为“本发明的化合物”）配制成易于使用的治疗剂量单位 包括人在内的哺乳动物的治疗（包括预防性治疗）。

公开(公告)号：WO2007023342A3

公开(公告)日：2007-03-01

申请号：PCT/IB2006/002169

申请日：2006-05-05

Applicant: MEDICHEM, S.A. ,  SERRANO, Jordi, Puig ,  ILLADO, Jordi Bosch

Inventor： SERRANO, Jordi, Puig ,  ILLADO, Jordi Bosch

IPC: C07F9/58 ,  A61K31/675 ,  A61P19/10

Abstract: This invention relates to the process of making geminal bisphosphonic acids and pharmaceutically acceptable salts and/or hydrates thereof which have the formula (I): wherein X 1 , X 2 , X 3 , X 1 R 1 and R 2 are described herein.

公开(公告)号：WO2007020533A2

公开(公告)日：2007-02-22

申请号：PCT/IB2006/002878

申请日：2006-05-05

Applicant: MEDICHEM, S.A. ,  ARNALOT AGUILAR, Carme

Inventor： ARNALOT AGUILAR, Carme

IPC: C07D403/10 ,  A61K31/4178 ,  A61P9/12

CPC classification number: C07D403/10

Abstract: The invention relates to the preparation of losartan and its salts (e.g., losartan potassium). More particularly, the invention relates to the preparation of losartan and its salts (e.g., losartan potassium) in a simplified process that provides higher purity losartan potassium and losartan potassium having larger crystal sizes. The invention further includes formulating losartan, its salts (e.g., losartan potassium ) and/or in vivo cleavable prodrugs thereof (collectively "the compounds of the invention") into readily usable dosage units for the therapeutic treatment (including prophylactic treatment) of mammals, including humans.

Abstract translation: 本发明涉及氯沙坦及其盐（如氯沙坦钾）的制备。 更具体地，本发明涉及以简化的方法制备氯沙坦及其盐（例如氯沙坦钾），其提供具有较大晶体尺寸的较高纯度的氯沙坦钾和氯沙坦钾。 本发明还包括将氯沙坦，其盐（例如氯沙坦钾）和/或其体内可切割前药（统称为“本发明化合物”）配制成用于哺乳动物的治疗性治疗（包括预防性治疗）的易用的剂量单位， 包括人类。

公开(公告)号：WO2005108394A1

公开(公告)日：2005-11-17

申请号：PCT/EP2004/005098

申请日：2004-05-12

Applicant: MEDICHEM S.A. ,  DURAN LÓPEZ, Ernesto ,  TOJO SUÁREZ, Gabriel

Inventor： DURAN LÓPEZ, Ernesto ,  TOJO SUÁREZ, Gabriel

IPC: C07D417/12

CPC classification number: C07D417/12

Abstract: The present invention relates to a process for the preparation of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxy]benzyl-2,4-thiazolidinedione of formula (I) (Rosiglitazone), which comprises the reaction of 5-{4-[2-(N-methyl-N-(2-pyridyl)amino)ethoxyl]benzylidene-2,4-thiazolidinedione of formula (II), with a 1,4-dihydropyridine of general formula (III).

Abstract translation: 本发明涉及式（I）的5- {4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]苄基-2,4-噻唑烷二酮的制备方法（罗格列酮） 其包括式（II）的5- {4- [2-（N-甲基-N-（2-吡啶基）氨基）乙氧基]亚苄基-2,4-噻唑烷二酮与1,4-二氢吡啶 的通式（III）。